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    Barbitúricos

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    KelletCadilloBarrueto
    Cyclobarbital is a hypnotic barbiturate used for its sedative and hypnotic properties. It is a white crystalline powder that is soluble in water and ethanol. Cyclobarbital is rapidly absorbed after oral administration and primarily metabolized by oxidation to ketocyclobarbital, with less than 10% excreted unchanged in urine. Therapeutic concentrations in plasma are typically 2-10 mg/L. The estimated minimum lethal dose is 2g and toxicity is associated with blood concentrations over 10mg/L.

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    Barbitúricos

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    KelletCadilloBarrueto
    96 views4 pages
    Cyclobarbital is a hypnotic barbiturate used for its sedative and hypnotic properties. It is a white crystalline powder that is soluble in water and ethanol. Cyclobarbital is rapidly absorbed after oral administration and primarily metabolized by oxidation to ketocyclobarbital, with less than 10% excreted unchanged in urine. Therapeutic concentrations in plasma are typically 2-10 mg/L. The estimated minimum lethal dose is 2g and toxicity is associated with blood concentrations over 10mg/L.

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    Barbitúricos (2)

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    Cyclobarbital is a hypnotic barbiturate used for its sedative and hypnotic properties. It is a white crystalline powder that is soluble in water and ethanol. Cyclobarbital is rapidly absorbed after oral administration and primarily metabolized by oxidation to ketocyclobarbital, with less than 10% excreted unchanged in urine. Therapeutic concentrations in plasma are typically 2-10 mg/L. The estimated minimum lethal dose is 2g and toxicity is associated with blood concentrations over 10mg/L.

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    96 views4 pages

    Barbitúricos

    Uploaded by

    KelletCadilloBarrueto
    Cyclobarbital is a hypnotic barbiturate used for its sedative and hypnotic properties. It is a white crystalline powder that is soluble in water and ethanol. Cyclobarbital is rapidly absorbed after oral administration and primarily metabolized by oxidation to ketocyclobarbital, with less than 10% excreted unchanged in urine. Therapeutic concentrations in plasma are typically 2-10 mg/L. The estimated minimum lethal dose is 2g and toxicity is associated with blood concentrations over 10mg/L.

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    of 4

    Barbitúricos

    Cyclobarbital
    Hypnotic, Barbiturate
    Synonyms. Ciclobarbital; Cyclobarbitalum; Cyclobarbitone; Ethylhexabital;
    Hexemalum; Tetrahydrophenobarbital.
    Proprietary names. Cavonyl; Cyclodorm; Cyklodorm; Fanodormo; Irifan; Namuron;
    Palinum; Phanodorm; Phanodorn; Philodorm; Prälumin; Pro-Sonil; Sonaform.

    Note.

    The name ciclobarbital has been applied to hexobarbital.

    5-(1-Cyclohexen–1–yl)-5–ethyl-2,4,6(1H,3H,5H)-pyrimidinetrione
    C12H16N2O3=236.3
    CAS—52–31–3

    A white crystalline powder, which gradually decomposes on storage. M.p. 171° to 174°.

    Soluble 1 in 800 of water, 1 in 5 of ethanol, 1 in 20 of chloroform, and 1 in 20 of ether.

    Cyclobarbital Calcium
    Synonyms. Ciclobarbital Calcium; Cyclobarbitone Calcium; Hexemalcalcium.
    Proprietary name. It is an ingredient of Domidorm.
    (C12H15N2O3)2Ca=510.6
    CAS-143–76–0

    A white or slightly yellowish, crystalline powder.

    Soluble 1 in 70 of water, 1 in 500 of 95% alcohol. Practically insoluble in ether and


    chloroform.
    Dissociation Constant.

    pKa7.6 (20°).

    Partition Coefficient.

    Log P(octanol/water), 1.77.

    Colour Tests.

    Koppanyi–Zwikker Test—violet; Mercurous Nitrate—black; Vanillin Reagent—


    brown–red/green.

    1.4 Procedimiento
    Se usarán los extractos obtenidos en el aislamiento de los T.O.F. y se procederá a realizar las diferentes
    reacciones de reconocimiento.

    . Rx de reconocimiento de Barbitúricos:

    - Rx de Parry-Coppangy

    * M.P. 5 mL.

    * Co(NO3)2 5% en EtOH III Gts.

    * Isopropilamin 5% en EtOH IV Gts.

    * Observar la coloración.

    - Rx de Zwiker:

    * M.P. 5 mL.

    * CuSO4 0.5% 0.5 mL.

    * Agitar fuertemente

    * Piridina 5% (CHCl3) 0.5 mL.

    * Observar coloración de la fase orgánica

    Thin–layer Chromatography.

    System TD—Rf 50; system TE—Rf 40; system TF—Rf 64; system TH—Rf 59; system
    TAD—Rf 58; system TAE—Rf 88. (Mercuric chloride–diphenylcarbazone reagent,
    positive; mercurous nitrate spray, black; acidified potassium permanganate solution,
    yellow–brown; Zwikker's reagent, pink.)
    Ultraviolet Spectrum.

    Borax buffer 0.05 M (pH 9.2)—239 nm (A11=410a); 1 M sodium hydroxide (pH 13)—
    256 nm (A11=320b).

    Disposition in the Body.

    Rapidly absorbed after oral administration. The main metabolic reaction appears to be
    oxidation to ketocyclobarbital [5-(3–oxocyclohex–1–enyl)-5–ethylbarbituric acid]. Less
    than 10% of a dose is excreted in the urine unchanged.

    THERAPEUTIC CONCENTRATION.
    In plasma, usually in the range 2 to 10 mg/L.

    After a single oral dose of 300 mg of the calcium salt, given to 6 subjects, peak plasma
    concentrations of 7.4 to 10.3 mg/L (mean 8.7) were attained in 0.7 to 2.5 h. [D. D.
    Breimer and A. C. M. Winten,Eur. J. Clin. Pharmacol.,1976, 9, 443–450.]

    TOXICITY.
    The estimated minimum lethal dose is 2 g. Severe toxic effects are associated with
    blood concentrations greater than 10 mg/L.

    HALF–LIFE.
    Plasma half–life, 8 to 17 h (mean 12), increased in subjects with liver disease.

    VOLUME OF DISTRIBUTION.
    About 0.5 L/kg.
    CLEARANCE.
    Plasma clearance, about 0.5 mL/min/kg.

    PROTEIN BINDING.
    In plasma, about 70%.

    Dose.

    100 to 400 mg of cyclobarbital calcium, as a hypnotic.

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